Composition containing sucrafate and a topical anesthetic for humans and animals and method of use thereof

ABSTRACT

A composition and method of treating plurality of conditions utilizes a combination of sucralfate and a topical anesthetic such as lidocaine. The composition finds utility in treating the symptoms of burns or mange and to relieve the associated irritations and discomfort.

REFERENCE TO RELATED APPLICATIONS

This application is a Continuation-in-Part Application of U.S. patentapplication Ser. No. 09/321,946 filed May 28, 1999, now patented U.S.Pat. No. 6,194,455 and U.S. patent application Ser. No. 09/779,384 filedFeb. 8, 2001 now patented U.S. Pat. No. 6,372,786.

BACKGROUND OF THE INVENTION

1. Field of the Invention

The instant invention relates generally to compositions for treatingskin ulcers, burns and mange and particularly to compositions for humanmedical or veterinary use containing sucralfate in combination with atopical anesthetic for treating a variety of medical conditions.

2. Description of the Related Art

Compositions containing sucralfate or topical anesthetics are known inthe art. For example, U.S. Pat. No. 5,246,697 (Conte, U. et al., 21 Sep.1993) discloses the use of a sucralfate-containing gel as a vehicle forthe application of drugs having topic activity.

U.S. Pat. No. 5,411,738 (Hind, H., 2 May 1995) discloses a compositionand method for alleviating associated with shingles utilizing thetopical administration of lidocaine.

U.S. Pat. No. 5,478,814 (Packman, E. W., 2 May 1995) discloses acomposition and method for treating hemorrhoids utilizing the topicaladministration of sucralfate in combination with a topically therapeuticagent, including an anesthetic.

U.S. Pat. No. 5,707,653 (Goldberg, A. H., 13 Jan. 1998) discloses acomposition for treating internal or external ulcers which containssucralfate in combination with an antibiotic.

U.S. Pat. No. 6,194,455 (Wharton, common inventor) discloses cure forskin ulcers.

SUMMARY OF THE INVENTION

The present invention is concerned with compositions for treating skinulcers, burns and mange and particularly to compositions for humanmedical or veterinary use containing sucralfate in combination with atopical anesthetic for treating a variety of medical conditions.

A primary object of the present invention is to provide a compositionand method for treating a wide variety of skin ulcers, burns and mangewhich utilizes a sucralfate in combination with a topical anestheticsuch as lidocaine.

Another object of the present invention is to provide a composition andmethod able to relieve irritations and discomfort caused by poison ivy,poison oak, poison sumac, bedsores, sore throats, burns, mange, surgicalincisions and skin ulcers on both humans on animals.

A further object of the present invention is to provide a compositionand method for preventing the formation of herpes ulcers.

An additional object of the present invention is to provide acomposition and method for promoting healing of diabetic ulcers.

Another object of the present invention is to provide a composition fortreating skin ulcers which contains sucralfate in combination with atopical anesthetic and an antibiotic.

A further object of the present invention is to provide a compositionand method for treating skin ulcers which provides both immediate relieffrom pain and long-lasting healing of the ulcer.

Another object of the present invention is to provide a composition andmethod for treating skin conditions such as acne, eczema, shingles,psoriasis, ringworm, jock itch, athlete's foot, burns, and abrasions,which contains sucralfate in combination with one or more antibiotics, atopical anesthetic, or both.

Still another object of the invention is to provide a composition andmethod for treating sinus conditions containing sucralfate incombination with a topical anesthetic such as lidocaine.

Still another object of the invention is to provide a composition andmethod for treating burns containing sucralfate in combination with atopical anesthetic such as lidocaine.

Still another object of the invention is to provide a composition andmethod for treating mange containing sucralfate in combination with atopical anesthetic such as lidocaine.

The foregoing and other objects, advantages and characterizing featureswill become apparent from the following description of certainillustrative embodiments of the invention.

The novel features which are considered characteristic for the inventionare set forth in the appended claims. The invention itself, however,both as to its construction and is method of operation, together withadditional objects and advantages thereof, will be best understood fromthe following description of the specific embodiments when read andunderstood in connection with the accompanying drawings. Attention iscalled to the fact, however, that the drawings are illustrative only,and that changes may be made in the specific construction illustratedand described within the scope of the appended claims.

BRIEF DESCRIPTION OF THE DRAWING FIGURES

Various other objects, features and attendant advantages of the presentinvention will become more fully appreciated as the same becomes betterunderstood when considered in conjunction with the accompanyingdrawings, in which like reference characters designate the same orsimilar parts throughout the several views.

FIG. 1 illustrates the chemical structure for sucralfate.

FIG. 2 illustrates the chemical structure for lidocaine.

DESCRIPTION OF THE PREFERRED EMBODIMENTS

Turning now descriptively to the drawings, in which similar referencecharacters denote similar elements throughout the several views, theFigures illustrate a composition for treating skin ulcers of the presentinvention. With regard to the reference numerals used, the followingnumbering is used throughout the various drawing figures.

-   10 chemical structure for sucralfate as an aluminum complex-   12 noncomplexed portion of 10-   14 identification of R-groups of 12 as -SO3Al(OH)2-   16 aluminum complex portion of 10-   definition of x and y from 16-   20 chemical structure of lidocaine-   22 chemical formula for lidocaine-   24 molecular weight of lidocaine

FIGS. 1 and 2 illustrate a composition for treating skin ulcers, burnsand mange of the present invention. In its broadest embodiment, thepresent invention comprises a topically-applicable composition includingsucralfate 10 and a topical anesthetic or an antibiotic.

Sucralfate is an a-D-glucopyranoside, §-D-fructofuranosyl-,octakis-(hydrogen sulfate), aluminum complex as illustrated in FIG. 1.It is sold under the trade name CARAFATEÒ, in both tablet and liquidsuspension form. It is most commonly dispensed for use in treatingduodenal ulcers. The present invention is based on the finding thatsucralfate, in combination with other active components such as topicalanesthetics, antibiotics, antioxidants, vitamins and the like, caneffectively treat a wide variety of topical conditions.

In preferred form, the composition of the invention includes sucralfateand lidocaine in combination. Lidocaine (Xylocaine), is an amideoriginally synthesized from cocaine, and is one of the most widely usedlocal anesthetics in use today. It is administered parenterally forventricular arrhythmias, subcutaneously for minor surgical procedures,and topically to mucosal surfaces prior to invasive procedures.Available forms include a topical solution (2-4%), a rectal suppository(10%), an aerosol (10%), a jelly (2%), viscous lidocaine (2%), and asolution for intravenous and subcutaneous administration (0.5-2%).

The sucralfate is normally provided in suspension form, at aconcentration of 1 g sucralfate per 10 ml of suspension. The preferredconcentrations for the present invention results from the combination of1 drop (about 0.1 g) of 2% lidocaine mixed together with about 0.25fluid ounces (about 7.5 ml) of sucralfate suspension. When mixed in thisproportion, the suspension thickens to the consistency of a gel,providing for ready administration to the patient.

Thus prepared, the composition of the present invention can be used toeffectively treat a wide range of skin ailments, providing pain reliefand promoting healing of any open ulcers. Additionally, further activecomponents may be added to the composition as needed. For example,antibiotics and/or antifungal agents, vitamins such as vitamins A, C andE, plants extracts such as aloe vera or other plant materials which maypromote healing, and combinations thereof.

Sucralfate binds preferentially to affected sites to form a protectivecoating thereon. Accordingly, the compositions of the present inventionprovide for the preferential delivery, to the wound site, of the variousactive components via the sucralfate in the composition. Theeffectiveness of the sucralfate in acting as a preferential carrier maybe enhanced when the active component has an affinity for sucralfate, asmany pharmaceutical products do. For example, the antibioticstetracycline, doxycycline, nalidixic acid, the fluoroquinoloneantibiotics ciprofloxacin, norfloxacin and ofloxacin, and the antifungalketoconazole all have been shown to have some affinity for sucralfateand may find particular utility in the compositions of the presentinvention.

In addition to these compounds which adsorb to the sucralfate, otherantibiotics also find utility in the compositions of the invention. Thisincludes sulfa drugs and other antibiotics such as bacitracin,trimethoprim, penicillin and erythromycin. A preferred antibiotic is acombination of trimethoprirm and sulfamethoxazole, in a weight ratio of1:5, respectively, sold under the tradename Bactrim™.

The composition has been used to treat effectively many differentailments. For example, it has been used effectively to relieve pain andpromote healing of diabetic ulcers, herpes ulcers, shingles, eczema,acne, psoriasis, skin rashes, burns and abrasions, and the like. Thecomposition is further used effectively to reirritations and discomfortcaused by poison ivy, poison oak, poison sumac, bedsores, soar throats,burns, surgical incisions and skin ulcers on humans, animals and mange.In each instance, immediate relief from the pain caused by the ulcers,and much more rapid healing of the wounds than when left untreated ortreated by conventional methods was reported in the case of humans andvisible in the case of animals and mange. The composition has also beenshown to be effective in treating sinus conditions where pain andinflammation are implicated. When used as a gargle, the composition hasproven effective in treating soar throats and minor throat irritationssuch as those caused by colds and flu.

The composition of the present invention has shown further, unexpectedutility in preventing the development of herpes ulcers. It has beenfound that, when the composition of the present invention is applied toa nascent herpes outbreak (when a small bump occurs on the skin, thetypical foreshadowing of an outbreak), the bump recedes within 1 ½ to 2days, then disappears without developing into a herpes ulcer.Additionally, patients report that after using the composition of theinvention to stem the outbreak, the time between outbreaks is greatlyextended, typically by a factor of 3 to 4. Therefore, the inventionprovides prophylactic utility for preventing herpes outbreaks. It isanticipated that such prophylactic utility extends also to otherrecurring conditions, such as psoriasis, diabetic ulcers, and the like.

The present invention can greatly alleviate the symptoms of chicken pox,and promotes the rapid healing of the associated skin eruptions suchthat scarring is avoided. The results are similar for treatment ofinfected skin rashes; pain relief was immediate and the skin appearedcompletely healed within 2 to 3 days.

In such conditions where antibiotics or antifungal agents are useful,the composition has also shown great efficacy. Such conditions include,for example, acne vulgaris, ringworm, jock itch, athlete's foot,conditions where infection is a concern, such as any open wounds, andthe like.

It will be understood that each of the elements described above, or twoor more together, may also find a useful application in other types ofapplications differing from the type described above. This includes, forexample, veterinary applications as well as the medical applicationsdescribed herein.

While the invention has been illustrated and described as embodied in acomposition for treating skin ulcers, it is not intended to be limitedto the details shown, since it will be understood that variousomissions, modifications, substitutions and changes in the forms anddetails of the formulation illustrated and in its operation can be madeby those skilled in the art without departing in any way from the spiritand scope of the present invention.

Without further analysis, the foregoing will so fully reveal the gist ofthe present invention that others can, by applying current knowledge,readily adapt it for various applications without omitting featuresthat, from the standpoint of prior art, fairly constitute essentialcharacteristics of this invention.

What is claimed as new and desired to be protected by Letters Patent isset forth in the appended claims.

1. The method of treating burns comprising the topical administration ofa gel comprising a pharmaceutically effective amount of sucralfate,lidocaine and a combination of trimethoprim and sulfamethoxazole whereinsucralfate and lidocaine in a weight ratio of sucralfate to lidocaine ina range of about 500:1 to about 200:1 in a pharmaceutically acceptablecarrier.
 2. The method as recited in claim 1, wherein said sucralfateand lidocaine are present in a weight:weight ratio of about 375:1,respectively.
 3. The method as recited in claim 1, wherein said methodis also used to treat burns and accelerating the healing of the burns.4. The method as recited in claim 3, wherein said composition furtherincludes aloe and vitamin E.
 5. The method as recited in claim 1,wherein said method comprising steps of mixing an aqueous suspension ofsucralfate, present in the concentration of 1 gram sucralfate per 10 mlof suspension, with a 2% lidocaine solution, then mixing until aresulting composition achieves a gel-like consistency, and then applyingto the affected area.
 6. The process as recited in claim 5, whereinabout 0.1 g of 2% lidocaine solution is added to each 7.5 ml ofsucralfate suspension.